Abstract

90501010 particle size is 0.5-1.5 μm; and the percent deposition of the particles with the aerodynamic particle size of 1.4-5.4 μm in the fudosteine inhalation solution is not less than 50%. In addition, further provided is a drug assembly for use in conjunction with the nebulization inhalation solution, comprising the inhalation composition, and a nebulizer and a nebulizing cup with specific parameters. The fudosteine nebulization inhalation solution composition and the assembly thereof have the advantages of a small effective dose, acting fast, high drug delivery efficiency, and the like, and are particularly effective in treating tracheal and main bronchial diseases.

IPC Classes  ?

• A61K 9/72 - Medicinal preparations characterised by special physical form for smoking or inhaling
• A61K 9/08 - Solutions
• A61K 31/198 - Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
• A61M 11/00 - Sprayers or atomisers specially adapted for therapeutic purposes
• A61M 15/00 - Inhalators
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 11/06 - Antiasthmatics
• A61P 11/10 - Expectorants
• A61P 31/06 - Antibacterial agents for tuberculosis

Abstract

A glucoside derivative, and a preparation method therefor and an application thereof. Specifically, provided is a glucoside derivative, which is a compound as represented by formula (I) or a pharmaceutically acceptable salt thereof. The glucoside derivative can be used for treatment of diabetes mellitus II or diabetes mellitus I.

IPC Classes  ?

• C07D 309/10 - Oxygen atoms
• C07D 309/02 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
• C07D 335/02 - Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 407/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
• C07D 409/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
• A61K 31/351 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
• A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
• A61K 31/382 - Heterocyclic compounds having sulfur as a ring hetero atom having six-membered rings, e.g. thioxanthenes
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

Abstract

Provided are a Rho kinase inhibitor, a method for preparing same and the uses thereof. The Rho kinase inhibitor designates a compound of Formula I, a stereoisomer thereof or pharmaceutically acceptable salt thereof. The Rho kinase inhibitor promotes endothelial cells and endothelin expression, prostenin expression, and vascular factors NO synthesis and secretion, has a promoting effect on proprostin expression independently of the doses used, shows lower toxicity, while being safer.

IPC Classes  ?

• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

The present invention pertains to the medical field and relates to a compound of formula (III), a stereoisomer or pharmaceutically acceptable salt thereof. The present invention also relates to a method for preparing the compound, a stereoisomer or pharmaceutically acceptable salt thereof, and the medical uses of an intermediate thereof. The intermediate of the compound, the stereoisomer or pharmaceutically acceptable salt thereof disclosed herein apply can be used as a drug intermediate for preventing or treating diabetes or as an intermediate for preparing an inhibitor of hyperglycaemia and hypoglycaemia.

IPC Classes  ?

• C07D 309/10 - Oxygen atoms
• C07D 335/02 - Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 407/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
• C07D 409/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07H 1/00 - Processes for the preparation of sugar derivatives
• C07G 3/00 - Glycosides

Abstract

Disclosed are a compound as represented by formula II, and an isomer or available salt thereof. Also disclosed specifically are a manufacturing method for the compound, and the isomer or available salt thereof, and an application of the compound, and the isomer or available salt thereof as a drug intermediate. The compound, and the isomer or available salt thereof can be used as an intermediate for preparing a drug for preventing or treating diabetes, or as an intermediate for preparing a drug for inhibiting rise of the blood sugar and lowering the blood sugar level.

IPC Classes  ?

• C07D 309/02 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
• A61K 31/351 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

Abstract

The present invention belongs to the field of medicine, and specifically relates to a compound of formula (I), an isomer or a pharmaceutical salt thereof. This present invention more specifically relates to a compound, a stereoisomer thereof or a method for preparing a pharmaceutical salt thereof, and the medical uses thereof. The compound, stereoisomer or pharmaceutically acceptable salt thereof disclosed herein may be used for preventing or treating diabetes, and for inhibiting hyperglycaemia and hypoglycaemia.

IPC Classes  ?

• C07D 309/10 - Oxygen atoms
• C07D 335/02 - Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 407/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
• C07D 409/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
• A61K 31/351 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
• A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
• A61K 31/382 - Heterocyclic compounds having sulfur as a ring hetero atom having six-membered rings, e.g. thioxanthenes
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

Abstract

Provided are an Rho kinase inhibitor, a method for preparing same and the uses thereof. The Rho kinase inhibitor designates a compound of formula (I), a stereoisomer or pharmaceutically acceptable salt thereof. The Rho kinase inhibitor promotes endothelial cells and endothelin expression, prostenin expression, and vascular factors NO synthesis and secretion, has a promoting effect on proprostin expression independently of the doses used, shows lower toxicity, while being safer.

IPC Classes  ?

• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• A61P 25/00 - Drugs for disorders of the nervous system

Abstract

Provided is a method for synthesizing a terbutaline intermediate. The method provided in the present invention uses a single menstruum, which can be recycled, to carry out a reaction, and has a simplified process and a simple post-treatment operation. In addition, a key step uses dibromohydantoin as a brominating agent. The method is green, environmentally-friendly and pollution-free, and the obtained product has a high purity and a considerable yield.

IPC Classes  ?

• C07C 45/63 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by introduction of halogenPreparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by substitution of halogen atoms by other halogen atoms
• C07C 49/84 - Ketones containing a keto group bound to a six-membered aromatic ring containing ether groups, groups, groups, or groups